Despite the significance of ABC transporters to cancer MDR has been well stated in vitro and in vivo, there are only limited agents like verapamil, valspodar, dofequidar, Ko143, MK571 have been developed as ABC transporter modulators [11, 12] but still with few success in clinical practice mainly for inefficiency, adverse side-effects, non-specificity and uncertain drug-interactions [13–15]. The gene discussed is ABCG2; the disease is cancer.